ES2274106T3 - Derivados de pirano como inhibidores tanto de ace como de nep. - Google Patents

Derivados de pirano como inhibidores tanto de ace como de nep. Download PDF

Info

Publication number: ES2274106T3
Authority: ES; Spain
Prior art keywords: alkyl; aryl; alkanoyl; carbocyclic; represent
Prior art date: 2001-09-21
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Expired - Lifetime

Application number

ES02779395T

Other languages

English (en)

Spanish (es)

Inventor

Cynthia Anne Fink

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Novartis AG

Original Assignee

Novartis AG

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2001-09-21

Filing date

2002-09-20

Publication date

2007-05-16

2002-09-20 Application filed by Novartis AG filed Critical Novartis AG

2007-05-16 Application granted granted Critical

2007-05-16 Publication of ES2274106T3 publication Critical patent/ES2274106T3/es

2022-09-20 Anticipated expiration legal-status Critical

Status Expired - Lifetime legal-status Critical Current

Links

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125000000217 alkyl group Chemical group 0.000 claims description 91
-1 trifluoromethoxy, amino Chemical group 0.000 claims description 86
239000001257 hydrogen Substances 0.000 claims description 47
229910052739 hydrogen Inorganic materials 0.000 claims description 47
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 38
150000003839 salts Chemical class 0.000 claims description 36
125000001589 carboacyl group Chemical group 0.000 claims description 32
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 29
125000003545 alkoxy group Chemical group 0.000 claims description 28
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 26
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 24
125000004487 4-tetrahydropyranyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 21
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125000003435 aroyl group Chemical group 0.000 claims description 4
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125000000842 isoxazolyl group Chemical group 0.000 claims description 4
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PWAPCRSSMCLZHG-UHFFFAOYSA-N cyclopentylidene Chemical group [C]1CCCC1 PWAPCRSSMCLZHG-UHFFFAOYSA-N 0.000 claims description 3
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125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 3
125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 3
125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 3
RFZOWZXFEPZCSB-OALUTQOASA-N (2s)-2-[[2-[[(2s)-2-acetylsulfanyl-2-(oxan-4-yl)acetyl]amino]-2-methylpropanoyl]amino]-3-(4-methoxyphenyl)propanoic acid Chemical compound C1=CC(OC)=CC=C1C[C@@H](C(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](SC(C)=O)C1CCOCC1 RFZOWZXFEPZCSB-OALUTQOASA-N 0.000 claims description 2
LNGBDVFWYVNQKZ-IRXDYDNUSA-N (2s)-3-(4-methoxyphenyl)-2-[[2-methyl-2-[[(2s)-2-(oxan-4-yl)-2-sulfanylacetyl]amino]propanoyl]amino]propanoic acid Chemical compound C1=CC(OC)=CC=C1C[C@@H](C(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](S)C1CCOCC1 LNGBDVFWYVNQKZ-IRXDYDNUSA-N 0.000 claims description 2
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OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides

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Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Biophysics (AREA)
Biochemistry (AREA)
General Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Urology & Nephrology (AREA)
Hospice & Palliative Care (AREA)
Vascular Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)
Plural Heterocyclic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Pyrane Compounds (AREA)
Saccharide Compounds (AREA)

ES02779395T 2001-09-21 2002-09-20 Derivados de pirano como inhibidores tanto de ace como de nep. Expired - Lifetime ES2274106T3 (es)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US32382501P	2001-09-21	2001-09-21
US323825P		2001-09-21

Publications (1)

Publication Number	Publication Date
ES2274106T3 true ES2274106T3 (es)	2007-05-16

Family

ID=23260883

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ES02779395T Expired - Lifetime ES2274106T3 (es)	2001-09-21	2002-09-20	Derivados de pirano como inhibidores tanto de ace como de nep.

Country Status (11)

Country	Link
US (2)	US7071169B2 (de)
EP (1)	EP1430045B1 (de)
JP (1)	JP4263095B2 (de)
CN (1)	CN1304415C (de)
AT (1)	ATE342261T1 (de)
BR (1)	BR0212899A (de)
CA (1)	CA2456281A1 (de)
DE (1)	DE60215368T2 (de)
ES (1)	ES2274106T3 (de)
PT (1)	PT1430045E (de)
WO (1)	WO2003027091A1 (de)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
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JP4263095B2 (ja)	2001-09-21	2009-05-13	ノバルティスアクチエンゲゼルシャフト	Ａｃｅおよびｎｅｐの両阻害剤としてのピラン誘導体
TW200900399A (en)	2003-10-01	2009-01-01	Speedel Experimenta Ag	Organic compounds
FI20040674A0 (fi) *	2004-05-12	2004-05-12	Orion Corp	Menetelmä tromboembolisten sairauksien estoon
RU2410118C2 (ru)	2004-12-15	2011-01-27	Зольвай Фармасьютиклз Гмбх	ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ ИНГИБИТОРЫ НЭП (НЕЙТРАЛЬНОЙ ЭНДОПЕПТИДАЗЫ), ИНГИБИТОРЫ ЭНДОГЕННОЙ ПРОДУЦИРУЮЩЕЙ ЭНДОТЕЛИН СИСТЕМЫ И ИНГИБИТОРЫ ГМГ (ГИДРОКСИМЕТИЛГЛУТАРИЛ)СоА РЕДУКТАЗЫ
US20060205625A1 (en) *	2005-02-18	2006-09-14	Solvay Pharmaceuticals Gmbh	Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and diuretics
ES2344800T3 (es) *	2005-02-18	2010-09-07	Solvay Pharmaceuticals Gmbh	Composiciones farmaceuticas que comprenden inhibidores de nep, inhibidores del sistema productor de endotelina endogena y diureticos.
TW200722424A (en)	2005-03-31	2007-06-16	Speedel Experimenta Ag	Substituted piperidines
EP1897879A3 (de)	2005-03-31	2008-06-11	Speedel Experimenta AG	2,4,5-Substituierte Piperidine als Renin-Inhibitoren
JP4047365B2 (ja)	2006-01-11	2008-02-13	生化学工業株式会社	シクロアルカンカルボキサミド誘導体及びその製造方法
WO2007080884A1 (ja) *	2006-01-11	2007-07-19	Seikagaku Corporation	シクロアルキルカルボニルアミノ酸エステル誘導体及びその製造方法
JP3975226B2 (ja)	2006-01-11	2007-09-12	生化学工業株式会社	シクロアルキルカルボニルアミノ酸誘導体及びその製造方法
EP2545920A1 (de) *	2007-08-22	2013-01-16	Abbott GmbH & Co. KG	Therapie für Diabeteskomplikationen
WO2009127251A1 (en) *	2008-04-16	2009-10-22	Novartis Ag	Combinations comprising a renin inhibitor
UY38072A (es)	2018-02-07	2019-10-01	Novartis Ag	Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
KR20210021457A (ko)	2018-05-14	2021-02-26	리아타 파마슈티컬즈, 아이엔씨.	열충격 단백질 경로와 연관된 질환의 치료를 위한 변형된 당기를 가진 바이아릴 아마이드

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JPH04211648A (ja) *	1990-07-27	1992-08-03	Nippon Kayaku Co Ltd	ケト酸アミド誘導体
US5432186A (en) *	1993-11-16	1995-07-11	Ciba-Geigy Corporation	Cyclic amino acid derivatives
ATE193706T1 (de) *	1993-11-16	2000-06-15	Novartis Ag	Zyklische aminosäure-derivate mit ace und nep inhibierender aktivität
CA2324251A1 (en) *	1998-04-23	1999-11-04	Novartis Ag	Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme
WO1999055726A1 (en) *	1998-04-23	1999-11-04	Novartis Ag	Certain thiol inhibitors of endothelin-converting enzyme
AU2001254776A1 (en)	2000-04-06	2001-10-23	Novartis Ag	Organic compounds
US6777443B2 (en) *	2001-05-15	2004-08-17	Novartis Ag	Dipeptide derivatives
JP4263095B2 (ja)	2001-09-21	2009-05-13	ノバルティスアクチエンゲゼルシャフト	Ａｃｅおよびｎｅｐの両阻害剤としてのピラン誘導体

2002
- 2002-09-20 JP JP2003530679A patent/JP4263095B2/ja not_active Expired - Fee Related
- 2002-09-20 CA CA002456281A patent/CA2456281A1/en not_active Abandoned
- 2002-09-20 WO PCT/EP2002/010608 patent/WO2003027091A1/en not_active Ceased
- 2002-09-20 BR BR0212899-3A patent/BR0212899A/pt not_active IP Right Cessation
- 2002-09-20 US US10/487,742 patent/US7071169B2/en not_active Expired - Fee Related
- 2002-09-20 DE DE60215368T patent/DE60215368T2/de not_active Expired - Lifetime
- 2002-09-20 EP EP02779395A patent/EP1430045B1/de not_active Expired - Lifetime
- 2002-09-20 ES ES02779395T patent/ES2274106T3/es not_active Expired - Lifetime
- 2002-09-20 PT PT02779395T patent/PT1430045E/pt unknown
- 2002-09-20 AT AT02779395T patent/ATE342261T1/de not_active IP Right Cessation
- 2002-09-20 CN CNB028183010A patent/CN1304415C/zh not_active Expired - Fee Related
2006
- 2006-05-01 US US11/414,906 patent/US20060194742A1/en not_active Abandoned

Also Published As

Publication number	Publication date
ATE342261T1 (de)	2006-11-15
DE60215368D1 (de)	2006-11-23
CA2456281A1 (en)	2003-04-03
EP1430045B1 (de)	2006-10-11
JP4263095B2 (ja)	2009-05-13
DE60215368T2 (de)	2007-08-16
US7071169B2 (en)	2006-07-04
EP1430045A1 (de)	2004-06-23
BR0212899A (pt)	2004-11-03
CN1304415C (zh)	2007-03-14
WO2003027091A1 (en)	2003-04-03
US20040266698A1 (en)	2004-12-30
CN1555372A (zh)	2004-12-15
PT1430045E (pt)	2007-01-31
JP2005504099A (ja)	2005-02-10
US20060194742A1 (en)	2006-08-31
HK1068332A1 (en)	2005-04-29

Publication	Publication Date	Title
US6777443B2 (en)	2004-08-17	Dipeptide derivatives
ES2274106T3 (es)	2007-05-16	Derivados de pirano como inhibidores tanto de ace como de nep.
AU2002314067A1 (en)	2003-05-01	Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors
US5508266A (en)	1996-04-16	Gem-disubstituted amino acid derivatives
EP0655461B1 (de)	2000-06-07	Zyklische Aminosäure-Derivate mit ACE und NEP inhibierender Aktivität
ES2237917T3 (es)	2005-08-01	Ciertos inhibidores tiolicos substituidos con heteroarilo de enzima conversora de endotelina.
US5432186A (en)	1995-07-11	Cyclic amino acid derivatives
ES2322263T3 (es)	2009-06-18	Mitroxiderivados de enalapril y compuestos relacionados con inhibidores de ace, para el tratamiento de enfermedades cardiovasculares.
EP0812205A1 (de)	1997-12-17	Antithrombotisch wirkende azacycloalkyl-alkanoyl-peptide und-pseudopeptide
US7910556B2 (en)	2011-03-22	PAR-2 agonist
HK1068332B (en)	2007-05-18	Pyrane derivatives as both ace- and nep-inhibitors
US20090215703A1 (en)	2009-08-27	PAR-2 Agonist
ZA200308590B (en)	2004-05-21	Dipeptide derivatives having a n-terminal 2-thiocyl group as vasopeptidase inhibitors.